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  1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. PKI-166

PKI-166 是一種高效、選擇性的,有口服生物活性的 EGFR 酪氨酸激酶抑制劑,IC50 值為 0.7 nM。

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PKI-166 Chemical Structure

PKI-166 Chemical Structure

CAS No. : 187724-61-4

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10 mM * 1 mL in DMSO ¥1650
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Other Forms of PKI-166:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM[1].

IC50 & Target

IC50: 0.7 nM (EGFR tyrosine kinase)[1]

體外研究
(In Vitro)

Pretreatment with PKI-166 (0-0.5 μM; 1 hour) inhibits EGFR autophosphorylation in human pancreatic cancer cells[1].
PKI-166 (0.03μ M; 6 days) enhanced the cytotoxicity mediated by gemcitabine[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: L3.6pl cells
Concentration: 0.01 μM, 0.05 μM, 0.5 μM
Incubation Time: 1 hour
Result: Inhibited EGFR autophosphorylation in a dose-dependent manner.

Cell Cytotoxicity Assay[1]

Cell Line: L3.6pl cells
Concentration: 0.03 μM
Incubation Time: 6 days
Result: Enhanced the cytotoxicity mediated by gemcitabine.
體內(nèi)研究
(In Vivo)

PKI-166 (100 mg/kg; p.o.; daily; day 7-day 35 after xenograft) inhibits of pancreatic cancer growth[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male athymic nude mice with L3.6pl cells xenograft (8–12 weeks)[1]
Dosage: 100 mg/kg
Administration: Oral administration; daily; from day 7 to day 35 after xenograft
Result: Significantly decreased median tumor volume.
分子量

330.38

Formula

C20H18N4O

CAS 號
性狀

固體

顏色

Off-white to light yellow

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實驗: 

DMSO 中的溶解度 : ≥ 125 mg/mL (378.35 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.0268 mL 15.1341 mL 30.2682 mL
5 mM 0.6054 mL 3.0268 mL 6.0536 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.58%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0268 mL 15.1341 mL 30.2682 mL 75.6704 mL
5 mM 0.6054 mL 3.0268 mL 6.0536 mL 15.1341 mL
10 mM 0.3027 mL 1.5134 mL 3.0268 mL 7.5670 mL
15 mM 0.2018 mL 1.0089 mL 2.0179 mL 5.0447 mL
20 mM 0.1513 mL 0.7567 mL 1.5134 mL 3.7835 mL
25 mM 0.1211 mL 0.6054 mL 1.2107 mL 3.0268 mL
30 mM 0.1009 mL 0.5045 mL 1.0089 mL 2.5223 mL
40 mM 0.0757 mL 0.3784 mL 0.7567 mL 1.8918 mL
50 mM 0.0605 mL 0.3027 mL 0.6054 mL 1.5134 mL
60 mM 0.0504 mL 0.2522 mL 0.5045 mL 1.2612 mL
80 mM 0.0378 mL 0.1892 mL 0.3784 mL 0.9459 mL
100 mM 0.0303 mL 0.1513 mL 0.3027 mL 0.7567 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

產(chǎn)品名稱:
PKI-166
目錄號:
HY-117155
需求量: